Proposing advancement criteria for efficient DMPK triage of new chemical entities.

abstract：:Since their initial isolation from the marine alga Delisea pulchra, bromofuranones have been investigated as potential inhibitors of quorum sensing (QS) in various bacterial strains. QS is an important mechanism by which bacteria co-ordinate their molecular response to the environment. QS is intrinsically linked to ba...

journal_title：Future medicinal chemistry

authors： Lyons T,Gahan CG,O'Sullivan TP

更新日期：2020-11-01 00:00:00

abstract：:CDK12 and CDK13 are Ser/Thr protein kinases that regulate transcription and co-transcriptional processes. Genetic silencing of CDK12 is associated with genomic instability in a variety of cancers, including difficult-to-treat breast, ovarian, colorectal, brain and pancreatic cancers, and is synthetic lethal with PARP,...

journal_title：Future medicinal chemistry

authors： Tadesse S,Duckett DR,Monastyrskyi A

更新日期：2021-01-01 00:00:00

abstract：:Sialic acid is associated with glycoproteins and gangliosides of eukaryotic cells. It regulates various molecular interactions, being implicated in inflammation and cancer, where its expression is regulated by sialyltransferases and sialidases. Angiogenesis, the formation of new capillaries, takes place during inflamm...

journal_title：Future medicinal chemistry

authors： Chiodelli P,Urbinati C,Paiardi G,Monti E,Rusnati M

更新日期：2018-12-01 00:00:00

abstract：AIM:There is little information available on the monoamine oxidase isoform selectivity of N-alkyl harmine analogs, which exhibit a myriad of activities including MAO-A, DYRK1A and cytotoxicity to several select cancer cell lines. RESULTS:Compounds 3e and 4c exhibited an IC50 of 0.83 ± 0.03 and 0.43 ± 0.002 μM against ...

journal_title：Future medicinal chemistry

authors： Haider S,Alhusban M,Chaurasiya ND,Tekwani BL,Chittiboyina AG,Khan IA

更新日期：2018-06-01 00:00:00

abstract：:Mitochondria play a key role in ATP generation, redox homeostasis and regulation of apoptosis. Due to the essential role of mitochondria in metabolism and cell survival, targeting mitochondria in cancer cells is considered as an attractive therapeutic strategy. However, metabolic flexibility in cancer cells may enable...

journal_title：Future medicinal chemistry

authors： Cui Q,Wen S,Huang P

更新日期：2017-06-01 00:00:00

abstract：:This review summarizes the basic milestones of the research of 5-azacytosine nucleosides chronologically from their discovery and anticancer activity identification, through to subsequent unveiling of their mechanism of action based on DNA hypomethylation and tumor-suppressor gene reactivation, to the final US FDA app...

journal_title：Future medicinal chemistry

authors： Krečmerová M,Otmar M

更新日期：2012-05-01 00:00:00

abstract：:The last 10 years have seen advances in automation and high-throughput biochemistry in the drug-discovery arena. However, these advances have not led to improvements in drug-discovery success. Drug programs must find new ways to identify superior compounds. Advances in label-free assay technologies may provide advanta...

journal_title：Future medicinal chemistry

authors： Lunn CA

更新日期：2010-11-01 00:00:00

abstract：:MRI has been recognized as one of the most applied medical imaging techniques in clinical practice. However, the presence of background signal coming from water protons in surrounding tissues makes sometimes the visualization of local contrast agents difficult. To remedy this, fluorine has been introduced as a reliabl...

journal_title：Future medicinal chemistry

authors： Hequet E,Henoumont C,Muller RN,Laurent S

更新日期：2019-05-01 00:00:00

abstract：:Computer-aided drug design (CADD) methodologies have made great advances and contributed significantly to the discovery and/or optimization of many clinically used drugs in recent years. CADD tools have likewise been applied to the discovery of inhibitors of HIV-1 integrase, a difficult and worthwhile target for the d...

journal_title：Future medicinal chemistry

authors： Liao C,Nicklaus MC

更新日期：2010-07-01 00:00:00

abstract：AIM:Cancer is among the leading causes of death worldwide. Medical interest has focused on macrocyclic polyamines because of their properties as antitumor agents. Results/Methodology: We have designed and synthesized a series of 1,2-diaminocyclohexane derivatives with notable in vitro antiproliferative activities again...

journal_title：Future medicinal chemistry

authors： Morales F,Ramírez A,Morata-Tarifa C,Navarro SA,Marchal JA,Campos JM,Conejo-García A

更新日期：2017-03-01 00:00:00

abstract：AIM:Research of the antitumor properties of biscationic compounds has received significant attention over the last few years. RESULTS:A novel family of 1,1'-([2,2'-bipyridine]-5,5'-diylbis(methylene))bis-substituted bromide (9a-k), containing two nitrogen atoms in the linker, considered as hypothetical hydrogen bond a...

journal_title：Future medicinal chemistry

authors： Castro-Navas FF,Schiaffino-Ortega S,Carrasco-Jimenez MP,Ríos-Marco P,Marco C,Espinosa A,Gallo MA,Mariotto E,Basso G,Viola G,Entrena-Guadix A,López-Cara LC

更新日期：2015-01-01 00:00:00

abstract：:During the current decade, data on the post-translational hydroxylation of specific amino acid residues of some ribosomal proteins and translation factors in both eukaryotes and eubacteria have accumulated. The reaction is catalyzed by dedicated oxygenases (so-called ribosomal oxygenases), whose action is impaired und...

journal_title：Future medicinal chemistry

authors： Graifer D,Malygin A,Karpova G

更新日期：2019-02-25 00:00:00

abstract：AIM:Currently, dozens of BRAF inhibitors and MEK inhibitors targeting RAF-MEK-ERK pathway have been introduced into clinical trials for cancer therapy. However, after 6-8 months of initial response, acquired drug resistance among the majority of those treated patients sharply diminished their clinical efficacy. DISCUS...

journal_title：Future medicinal chemistry

authors： Yu Z,Ye S,Hu G,Lv M,Tu Z,Zhou K,Li Q

更新日期：2015-01-01 00:00:00

abstract：AIM:Cisplatin resistance in ovarian cancer remains a complex problem as tumors frequently develop resistance against drugs, a mechanism sometimes mediated by ATP-Binding Cassette transporters. Our goal was to find compounds restricting their inhibition capacity to the cisplatin efflux mediated by ABCC2 pump, among prev...

journal_title：Future medicinal chemistry

authors： Comsa E,Nguyen KA,Loghin F,Boumendjel A,Peuchmaur M,Andrieu T,Falson P

更新日期：2018-06-01 00:00:00

abstract：:Chronic obstructive pulmonary disease (COPD) is one of the leading causes of death in the world today. Bronchodilators, particularly muscarinic antagonists and β(2) agonists, are recommended for patients with moderate to severe COPD. Dual-pharmacology muscarinic antagonist- β(2) agonist (MABA) molecules present an exc...

journal_title：Future medicinal chemistry

authors： Hughes AD,Jones LH

更新日期：2011-10-01 00:00:00

abstract：:Aim: With the increasing emergence of drug-resistant bacteria, the need for new antimicrobial agents has become extremely urgent. This work was to develop sulfonyl thiazoles as potential antibacterial agents. Results & methodology: Novel hybrids of sulfonyl thiazoles were developed from commercial acetanilide and acet...

journal_title：Future medicinal chemistry

authors： Hu YY,Wang J,Li TJ,Yadav Bheemanaboina RR,Ansari MF,Cheng Y,Zhou CH

更新日期：2020-10-01 00:00:00

abstract：:An accelerated rate of natural-product discovery is critical for the future of ion channel pharmacology. For the full potential of natural products to be realized, an interdisciplinary initiative is required that combines chemical ecology and ion channel physiology. A prime source of future drug leads targeted to ion ...

journal_title：Future medicinal chemistry

authors： Teichert RW,Olivera BM

更新日期：2010-05-01 00:00:00

abstract：AIM:Due to the complex nature of Alzheimer's disease, there is a renewed search for pleiotropic agents. RESULTS:Purine+coumarin hybrids have been synthesized and tested for the potential treatment of Alzheimer's disease. Hybrids 6, 4a-b, 14c and 14e inhibit significantly soybean lipoxygenase, whereas derivatives 14b, ...

journal_title：Future medicinal chemistry

authors： Kallitsakis MG,Yañez M,Soriano E,Marco-Contelles J,Hadjipavlou-Litina DJ,Litinas KE

更新日期：2015-01-01 00:00:00

abstract：:Clinical development in brain diseases has one of the lowest success rates in the pharmaceutical industry, and many promising rationally designed single-target R&D projects fail in expensive Phase III trials. By contrast, successful older CNS drugs do have a rich pharmacology. This article will provide arguments sugge...

journal_title：Future medicinal chemistry

authors： Geerts H,Kennis L

更新日期：2014-01-01 00:00:00

abstract：:Aim: To encapsulate amphotericin B (AmB) with reduced toxicity and comparable activity. Results & methodology: The α-linolenic acid (ALA)-modified monomethoxy polyethylene glycol-g-PEI-g-ALA conjugate was employed to prepare AmB-loaded micelles (AmB-M). In vitro activity and release behavior of AmB-M were investigated...

journal_title：Future medicinal chemistry

authors： Xu H,Teng F,Zhou F,Zhu L,Wen Y,Feng R,Song Z

更新日期：2019-10-01 00:00:00

abstract：:Graphical abstract [Formula: see text]. ...

journal_title：Future medicinal chemistry

authors： Choudhary S,Silakari O

更新日期：2020-02-01 00:00:00

abstract：:Hepatitis B Virus (HBV) is one of the most prevalent viral infections of human worldwide. The therapies are limited in the clinical context because of negative side effects of interferons and the development of viral resistance to the nucleoside/nucleotide inhibitors. In this review, we summarize the recent advances i...

journal_title：Future medicinal chemistry

authors： Jia H,Rai D,Zhan P,Chen X,Jiang X,Liu X

更新日期：2015-01-01 00:00:00

abstract：:More research effort needs to be invested in antimicrobial drug development to address the increasing threat of multidrug-resistant organisms. The enzyme DHPS has been a validated drug target for over 70 years as the target for the highly successful sulfa drugs. The use of sulfa drugs has been compromised by the wides...

journal_title：Future medicinal chemistry

authors： Hammoudeh DI,Zhao Y,White SW,Lee RE

更新日期：2013-07-01 00:00:00

abstract：:Cancer is a major devastating disease, and is a leading cause of death worldwide. Despite the progress in cancer treatment, cancer mortality rate remains high. Therefore, the discovery and development of improved anticancer drugs to treat cancer are needed. 4H-chromenes have strong cytotoxicity against a panel of huma...

journal_title：Future medicinal chemistry

authors： Patil SA,Patil R,Pfeffer LM,Miller DD

更新日期：2013-09-01 00:00:00

abstract：BACKGROUND:Benzimidazole derivatives are promising compounds for the treatment of parasitic infections. The structure-activity relationships of 91 benzimidazoles with activity against Trichomonas vaginalis and Giardia intestinalis were analyzed using a novel activity landscape modeling approach. RESULTS:We identified ...

journal_title：Future medicinal chemistry

authors： Aguayo-Ortiz R,Pérez-Villanueva J,Hernández-Campos A,Castillo R,Meurice N,Medina-Franco JL

更新日期：2014-03-01 00:00:00

abstract：:Alzheimer's disease (AD) is the most common cause of dementia with no cure at present. Cholesterol metabolism is closely associated with AD at several stages. ACAT1 converts free cholesterol to cholesteryl esters, and plays important roles in cellular cholesterol homeostasis. Recent studies show that in a mouse model,...

journal_title：Future medicinal chemistry

authors： Shibuya Y,Chang CC,Chang TY

更新日期：2015-01-01 00:00:00

abstract：:Every organism is in contact with numerous small molecules (<1000 Da). Chemicals may cause or trigger adverse health effects, including diseases of the immune system. They may also be exploited as drugs. In this review, we look at the interaction between small molecules and the immune system. We discuss the hapten and...

journal_title：Future medicinal chemistry

authors： Kadow S,Jux B,Chmill S,Esser C

更新日期：2009-12-01 00:00:00

abstract：:Bromodomain and extra-terminal domain (BET) protein family plays an important role in regulating gene transcription preferentially at super-enhancer regions and has been involved with several types of cancers as a candidate. Up to now, there are 16 pan-BET inhibitors in clinical trials, however, most of them have unde...

journal_title：Future medicinal chemistry

authors： Yang Y,Wu Z,Chen P,Zheng P,Zhang H,Zhou J

更新日期：2020-09-01 00:00:00

abstract：:Aim: The orphan drug auranofin was recently found to exhibit antimicrobial properties. Materials & methods: We explored the efficacy of auranofin by evaluating the minimal inhibitory concentration against a collection of over 500 clinical isolates derived from multiple institutions, inclusive of drug resistant strains...

journal_title：Future medicinal chemistry

authors： Tharmalingam N,Ribeiro NQ,da Silva DL,Naik MT,Cruz LI,Kim W,Shen S,Dos Santos JD,Ezikovich K,D'Agata EM,Mylonakis E,Fuchs BB

更新日期：2019-06-01 00:00:00

abstract：:The rise of antibiotic resistant bacteria requires unconventional strategies toward efficient chemotherapeutic agents, preferably with alternative mechanisms of action. The bacterial cell membrane has become an appealing target since its essential and highly conservative structure are key challenges to resistance mech...

journal_title：Future medicinal chemistry

authors： Dias C,Rauter AP

更新日期：2019-02-25 00:00:00